[go: up one dir, main page]

BR0113344A - Aza amino acid derivatives (factor xa inhibitors 15) - Google Patents

Aza amino acid derivatives (factor xa inhibitors 15)

Info

Publication number
BR0113344A
BR0113344A BR0113344-6A BR0113344A BR0113344A BR 0113344 A BR0113344 A BR 0113344A BR 0113344 A BR0113344 A BR 0113344A BR 0113344 A BR0113344 A BR 0113344A
Authority
BR
Brazil
Prior art keywords
inhibitors
factor
amino acid
acid derivatives
aza amino
Prior art date
Application number
BR0113344-6A
Other languages
Portuguese (pt)
Inventor
Werner Mederski
Horst Juraszyk
Dieter Dorsch
Christos Tsaklakidis
Johannes Gleitz
Christopher Barnes
Original Assignee
Merck Patent Gmbh
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of BR0113344A publication Critical patent/BR0113344A/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/47—Y being a hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/42—Y being a hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C333/00—Derivatives of thiocarbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C333/02—Monothiocarbamic acids; Derivatives thereof
    • C07C333/04—Monothiocarbamic acids; Derivatives thereof having nitrogen atoms of thiocarbamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40—Oxygen atoms
    • C07D211/44—Oxygen atoms attached in position 4
    • C07D211/46—Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D317/34—Oxygen atoms
    • C07D317/40—Vinylene carbonate; Substituted vinylene carbonates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)

Abstract

"DERIVADOS DE AZA AMINO áCIDO (INIBIDORES 15 DE FATOR X~ a~)". A invenção refere-se a semicarbazidas da fórmula geral I onde R^ 1^, R^ 2^, R^ 3^, R^ 4^ e I têm os significados indicados na reivindicação 1. Os compostos da fórmula I podem ser empregados como compostos ativos farmacêuticos em medicina humana e veterinária, em particular para o controle e prevenção de distúrbios tromboembólicos tais como trombose, infarto de miocárdio, arterioesclerose, inflamação, apoplexia, angina pectoris, restenose depois de angioplastia e claudicação intermitente."AZA ACID AMINO DERIVATIVES (FACTOR 15 INHIBITORS X ~ a ~)". The invention relates to semicarbazides of the general formula I wherein R 1, R 2, R 3, R 4 and I have the meanings indicated in claim 1. The compounds of formula I may be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, myocardial infarction, arteriosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty and intermittent claudication.

BR0113344-6A 2000-08-21 2001-08-21 Aza amino acid derivatives (factor xa inhibitors 15) BR0113344A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10040783A DE10040783A1 (en) 2000-08-21 2000-08-21 AZA amino acid derivatives (factor X¶a¶ inhibitors 15)
PCT/EP2001/009667 WO2002016315A1 (en) 2000-08-21 2001-08-21 Aza-amino acid derivatives (factor xa-inhibitors 15)

Publications (1)

Publication Number Publication Date
BR0113344A true BR0113344A (en) 2003-07-15

Family

ID=7653121

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0113344-6A BR0113344A (en) 2000-08-21 2001-08-21 Aza amino acid derivatives (factor xa inhibitors 15)

Country Status (19)

Country Link
US (1) US6849626B2 (en)
EP (1) EP1311476B1 (en)
JP (1) JP2004517811A (en)
KR (1) KR20030029810A (en)
CN (1) CN1469860A (en)
AR (1) AR030376A1 (en)
AT (1) ATE291012T1 (en)
AU (2) AU2001282113B2 (en)
BR (1) BR0113344A (en)
CA (1) CA2415838A1 (en)
CZ (1) CZ2003414A3 (en)
DE (2) DE10040783A1 (en)
ES (1) ES2238468T3 (en)
HU (1) HUP0303694A3 (en)
MX (1) MXPA03001555A (en)
NO (1) NO20030796D0 (en)
PL (1) PL360388A1 (en)
WO (1) WO2002016315A1 (en)
ZA (1) ZA200302252B (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10036852A1 (en) * 2000-07-28 2002-02-07 Merck Patent Gmbh urethane
US6660737B2 (en) 2001-05-04 2003-12-09 The Procter & Gamble Company Medicinal uses of hydrazones
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7232924B2 (en) 2001-06-11 2007-06-19 Xenoport, Inc. Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7186855B2 (en) 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
JP2005519114A (en) * 2002-03-04 2005-06-30 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング Semicarbazide derivatives and their use as antithrombotic agents
DE10220048A1 (en) * 2002-05-04 2003-11-13 Merck Patent Gmbh Semicarbazidderivate
UY27813A1 (en) 2002-05-31 2003-12-31 Smithkline Beecham Corp PEPTIDE-DISFORMILASE INHIBITORS
TW200410921A (en) * 2002-11-25 2004-07-01 Hoffmann La Roche Mandelic acid derivatives
DE10325962A1 (en) * 2003-06-07 2004-12-23 Merck Patent Gmbh Aroylsemicarbazidderivate
UA108596C2 (en) 2007-11-09 2015-05-25 Peptide deformylase inhibitors
JPWO2009096198A1 (en) * 2008-02-01 2011-05-26 一般社団法人ファルマＩｐ New biaryl derivatives

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3285957A (en) * 1964-02-13 1966-11-15 Monsanto Co Diphenyl semicarbazides
CN1268116A (en) 1997-08-27 2000-09-27 橘生药品工业株式会社 3-amidinoaniline derivatives activated blood coagulation factor X inhibitors, and intermediates for producing both

Also Published As

Publication number Publication date
HUP0303694A3 (en) 2006-02-28
EP1311476B1 (en) 2005-03-16
PL360388A1 (en) 2004-09-06
AU2001282113B2 (en) 2006-08-24
EP1311476A1 (en) 2003-05-21
KR20030029810A (en) 2003-04-16
AR030376A1 (en) 2003-08-20
DE10040783A1 (en) 2002-03-07
MXPA03001555A (en) 2003-06-06
NO20030796L (en) 2003-02-20
DE50105634D1 (en) 2005-04-21
CZ2003414A3 (en) 2003-08-13
WO2002016315A1 (en) 2002-02-28
ATE291012T1 (en) 2005-04-15
NO20030796D0 (en) 2003-02-20
ZA200302252B (en) 2004-06-28
HUP0303694A2 (en) 2004-03-01
JP2004517811A (en) 2004-06-17
ES2238468T3 (en) 2005-09-01
AU8211301A (en) 2002-03-04
US6849626B2 (en) 2005-02-01
US20040034072A1 (en) 2004-02-19
CN1469860A (en) 2004-01-21
CA2415838A1 (en) 2002-02-28

Similar Documents

Publication Publication Date Title
BR0113344A (en) Aza amino acid derivatives (factor xa inhibitors 15)
NZ529874A (en) Aromatic dicarboxylic acid derivatives useful as HDAC inhibitors
Rakesh et al. Quinazolinones linked amino acids derivatives as a new class of promising antimicrobial, antioxidant and anti-inflammatory agents
RU94040163A (en) Heterocyclic derivatives of carboxylic acid and their salts and pharmaceutical composition exhibiting antifibrotic activity or activity inhibiting prolylhydroxylase or collagen biosynthesis
NO20044731L (en) Quinoline and Isoquinoline Derivatives Process for Preparation thereof and its Use as Inflammatory Inhibitors
ES2196917T3 (en) HETEROAROMATIC AMIDES AS INHIBITORS OF FACTOR XA`.
BRPI0416692A (en) heterocyclic mek inhibitors and methods of using these
BR9916930A (en) Aromatic heterocyclic compounds as anti-inflammatory agents
NO20072595L (en) 3 arylaminopyridinderivater
HRP20020182B1 (en) Benzamide formulation with histone deacetylase inhibitor activity
GB9902453D0 (en) Chemical compounds
BRPI0415437A (en) compound, process for the preparation and use thereof, pharmaceutical composition, process for the preparation thereof, and, product
YU48803A (en) Tetrahydropyridine derivatives, their preparation and their use as cell proliferation inhibitors
NO20044744L (en) Carbamic acid compounds comprising a piperazine link as HDASin inhibitors
BR0111383A (en) 1,2,4-tri-substituted benzenes as 15-lipoxygenase inhibitors
TR200401962T4 (en) Heteroaromatic carboxamide derivatives and their use as inhibitors of the enzyme IKK-2
IL151459A0 (en) Novel malonic acid derivatives, processes for their preparation, their use as inhibitors of factor xa activity and pharmaceutical compositions containing them
MY144659A (en) 2-hydroxy-3-heteroarylindole derivatives as gsk3 inhibitors
ITMI20011733A0 (en) HYDROXAMIC ACID DERIVATIVES INHIBITORS OF HISTONE DEACETYLASE ENZYMES, AS NEW ANTI-INFLAMMATORY DRUGS INHIBITING THE SYNTHESIS OF CITOC
PT1005453E (en) SUBSTITUTED BENZENE COMPOUNDS AS ANTIPROLIFERATIVE REDUCING AGENTS
BR0311535A (en) Use of substituted cyanopyrrolidines and combination preparations containing them for the treatment of hyperlipidemia and associated diseases
DE60305113D1 (en) Boric acid salts and their use in the provision of drugs for thrombosis treatment
AU4888401A (en) Sulfonamide derivative as a matrix metalloproteinase inhibitor
DE60214569D1 (en) ULEARIC COMPOUNDS WITH ANTIPROTEOLYTIC EFFECT
BR0008310A (en) Alpha-Alanine derivatives

Legal Events

Date Code Title Description
B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]